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MN58b is a selective choline kinase α (CHKα) inhibitor that inhibits phosphorylcholine synthesis.It reduces cell growth by inducing apoptosis and has antitumor activity. | [in vitro]
The IC 50 s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 μM and 0.77 μM, respectively.
It has a marked effect on colony formation at 1 μM, and growth is completely abolished at 5 μM in all the cell lines.
It induces apoptosis and this response correlates with CHKα expression. Cell Viability Assay | Cell Line: | SK-PC-1 , Suit2 008, IMIM-PC2, and RWP-1 cells | | Concentration: | 1 μM, 5 μM | | Incubation Time: | 72 hours | | Result: | Inhibited ce lls growth. | Apoptosis Analysis | Cell Line: | SK-PC-1, Suit2 008, IMIM-PC2, and RWP -1 cells | | Concentration: | 1 μM, 2 μM, 5 μM, 10 μM | | Incubation Time: | 24 and 48 hours | | Result: | Induced cell apoptosis. | < /span> | [in vivo]
MN58b (4 mg/kg; intraperitoneal injection; once a day; for 5 days; MF-1 nude mice) treatment significantly decreases phosphomonoesters in both HT29 and MDA-MB-231 xenografts. Phosphocholine levels are found to correlate with choline kinase activities. | Animal Model: | MF-1 nude mice with HT29 or MDA-MB-231 cells | | Dosage: | 4 mg/kg | | Administration: | Intraperitoneal injection; once a day; for 5 days | | Result : | Phosphomonoesters decreased significantly. | | [target]
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DC Chemicals
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021-58447131 13564518121 |
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https://www.chemicalbook.com/ShowSupplierProductsList927327/0.htm |
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